Formulary
Varenicline: Indications, Dosing, Side Effects and Interactions
Varenicline is a selective nicotine-receptor partial agonist.
MedNext Academy | 3 min read
Varenicline: Indications, Dosing, Side Effects and Interactions
Varenicline is a selective nicotine-receptor partial agonist.
Drug action
Varenicline is a selective nicotine-receptor partial agonist.
Indications and dose
**To aid smoking cessation**
- **Adult** (By Mouth): Initially 500 micrograms once daily for 3 days, increased to 500 micrograms twice daily for 4 days, then 1 mg twice daily for 11 weeks; reduced if not tolerated to 500 micrograms twice daily, usually to be started 1-2 weeks before target stop date but can be started up to a maximum of 5 weeks before target stop date, 12-week course can be repeated in abstinent individuals to reduce risk of relapse.
Cautions
Conditions that may lower seizure threshold; history of cardiovascular disease; history of psychiatric illness (may exacerbate underlying illness including depression); predisposition to seizures
Side effects
Common or very common Appetite abnormal; asthenia; chest discomfort; constipation; diarrhoea; dizziness; drowsiness; dry mouth; gastrointestinal discomfort; gastrointestinal disorders; headache; joint disorders; muscle complaints; nausea; oral disorders; pain; skin reactions; sleep disorders; vomiting; weight increased Uncommon Allergic rhinitis; anxiety; arrhythmias; behaviour abnormal; burping; conjunctivitis; depression; eye pain; fever; fungal infection; haemorrhage; hallucination; hot flush; hyperglycaemia; influenza like illness; malaise; menorrhagia; mood swings; numbness; palpitations; seizure; sexual dysfunction; suicidal ideation; sweat changes; thinking abnormal; tinnitus; tremor; urinary disorders Rare or very rare Angioedema; bradyphrenia; coordination abnormal; costochondritis; cyst; diabetes mellitus; dysarthria; eye disorders; feeling cold; glycosuria; muscle tone increased; polydipsia; psychosis; scleral discolouration; severe cutaneous adverse reactions (SCARs); snoring; vaginal discharge; vision disorders Frequency not known Loss of consciousness
Interactions
**Severe interactions:**
- In patients with severe renal impairment, the concomitant use of cimetidine and Varenicline should be avoided.
- Nicotine replacement therapy (NRT) When Varenicline and transdermal NRT were co-administered to smokers for 12 days, there was a statistically significant decrease in average systolic blood pressure...
**Other interactions (17):**
- Based on Varenicline characteristics and clinical experience to date, Varenicline has no clinically meaningful drug interactions.
- No dosage adjustment of Varenicline or co-administered medicinal products listed below is recommended.
- Furthermore since metabolism of Varenicline represents less than 10% of its clearance, active substances known to affect the cytochrome P450 system are unlikely to alter the pharmacokinetics of...
- In vitro studies demonstrate that Varenicline does not inhibit human renal transport proteins at therapeutic concentrations.
- Metformin Varenicline did not affect the pharmacokinetics of metformin.
- Metformin had no effect on Varenicline pharmacokinetics.
Pregnancy
Avoid-toxicity in animal studies.
Breast feeding
Avoid-present in milk in animal studies.
Renal impairment
Dose adjustments If creatinine clearance less than 30 mL/minute, initial dose 500 micrograms once daily, increased after 3 days to 1 mg once daily. M See Prescribing in renal impairment .
Medicinal forms
Tablet
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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